Anticancer efficacy and selectivity are two critical factors for successful anti-cancer treatment. The classical approach for anticancer drug discovery is the use of cytotoxicity as a drug selection marker. However, the drug candidates identified via this approach usually show little selectivity to cancer versus normal tissues. As a result, the selected compounds fail to be developed for use as anticancer drugs because of their high toxicity to normal cells and tissues. An additional challenge in anticancer drug discovery and development is that cytotoxicity-based screening of chemical compound libraries over the past several decades has derived overwhelming numbers of compounds that show inhibition of cancer cell growth in vitro. However, identification of compounds that can exhibit clinically relevant anti-cancer effect in relevant animal models has proven very difficult. Thus, there is an ongoing and unmet need to identify and develop existing compounds so that they can be used for inhibition of cancer growth in clinically relevant treatment modalities. The present invention meets these and other needs.